BU08028 is a drug which acts as a potent
partial agonist
In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic e ...
at both the
μ-opioid receptor
The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical Π...
and
nociceptin receptor
The nociceptin opioid peptide receptor (NOP), also known as the nociceptin/orphanin FQ (N/OFQ) receptor or kappa-type 3 opioid receptor, is a protein that in humans is encoded by the ''OPRL1'' (opioid receptor-like 1) gene. The nociceptin receptor ...
. It is a
homologue of
buprenorphine
Buprenorphine is an opioid used to treat opioid use disorder, acute pain, and chronic pain. It can be used under the tongue (sublingual), in the cheek (buccal), by injection (intravenous and subcutaneous), as a skin patch (transdermal), ...
extended by just one carbon on the side chain, but has relatively greater activity at the nociceptin receptor, which is thought to reduce the abuse potential without compromising analgesia.
See also
*
BU-48
BU-48 is a drug that is used in scientific research. It is from the oripavine family, related to better-known drugs such as etorphine and buprenorphine.
The parent compound from which BU-48 was derived (with ''N''-methyl rather than methylcyclo ...
*
BU72
BU72 is an extremely potent opioid, with one of the highest known affinities for the μ-opioid receptor. In animal studies, it was found to be a potent analgesic, with a slow onset and long duration of action, but was not considered suitable to ...
References
{{pharm-stub
Mu-opioid receptor agonists
Heterocyclic compounds with 6 rings
Oxygen heterocycles
Nitrogen heterocycles
Cyclopropanes
Alcohols